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Name: Ethanol Name: Disulfiram (Antabuse)

Class: Alcohol
Mech.: Disordering of lipid memb. → perturbs fxns of ion-channels & other proteins. May augment Class: Aversive Agent
GABA med. synaptic inhib & Cl- influx. High conc → ↑ Cl- permeability w/o GABA mediation. Mech.: Irreversibly inactivates aldehyde dehydrogenase.
Absorption: Rapidly, and usu. completely, absorbed from mouth, stomach, small intestine.
Dist.: Rel. uniform distribution throughout all tissues and fluids. Absorption:
Metab.: 90-98% completely oxid. Zero order kinetics: 7-15 gram (1 drink)/hr. Mostly oxid. in liver Dist.:
by alcohol dehydrogenase. Resulting acetaldehyde oxid by mitoch. aldehyde dehydrog.
Excretion, t_: 2-10% not oxidized (excreted via lungs and kidneys). Metab.:
Tox./S.E.s: CNS—depressant (additive w/other depressants); Heart—↓ contractility, arrhythmia; Excretion, t_: Effective for 2-3 days.
Smooth Musc—vasodilation. May inhib. metab. of other drugs. Resp. depression, hypoglycemia.
Chronic S.E.s: Liver/GI—liver fat accum, hepatitis, fibrosis, cirrhosis; ↑ gastric & pancreatic Toxicity/S.E.s: Dizziness, metallic taste, nausea, headache, skin reactions.
secretion & mucosal damage → ↑ risk of gastritis and pancreatitis, aggravation of PUD. Nerv. Utility: Used to treat alcoholism. When alcohol is ingested, blood acetaldehyde
sys—symm. periph. nerve injury, memory loss, sleep disturbances, psychoses. concentrations rise, producing hangover symptoms of flushing, headache,
Blood—mild anemia (↓ prolif. of marrow cells), ↑ HDL/LDL ratio (↓ risk of CHD). nausea, vomiting, and hypotension.
CV—cardiomyopathy, arrhythmia. Fetal Alcohol Synd. Sex—impotence, sterility, testicular
atrophy, gynecomastia, ↓ estrogen metab. ↑ Cancer risk—mouth, pharynx, larynx, Special Features:
esophagus, liver, breast. Alcohol W/drawal Synd.
Utility: Solvent for drug admin., nerve blocking agent for pain relief, antidote for methanol and
ethylene glycol poisoning.
Special Features: Induces cyt. P450. Acute tolerance can occur.

Name: Methylphenidate (Ritalin) Name: Cocaine (Various)


Class: CNS Stimulant Class: CNS Stimulant (Indirect Sympathomimetic Agent)/Local Anesth (Ester)
Mech.: CNS Mech. = Release of DA, NE, & 5HT from nerve terminals. Some Mech.: Inhib. reuptake of catecholamines (DA, NE, 5HT) → prolonged action. Local anesthetic
properties from block of Na+ & Ca2+ channels → ↓ rate of rise of action potential, failure to
blockade of reuptake of DA, NE, & 5HT. Weak inhib. of MAO. Produces
propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more
elev. of mood, euphoria, ↑ alertness, ↓ sense of fatigue, ↓ food intake, easily blocked and remain blocked longer.
periph. sympathomimetic effects. Absorption: : Rapidly absorbed IV & oral. IV absorption can be limited w/a vasoconstrictor. Rapid
Absorption: Oral → good bioavail. topical absorption at mucous membranes.
Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart
Dist.: Crosses BBB. Metab.: Rapidly metab. by plasma pseudocholinesterases. Med. duration of anesth action.
Metab.: Toxicity/S.E.s: Fever, nausea, vomiting, confusion, headache. Neurosis, paranoia, frank psychosis.
Excretion, t_: Tolerance, but not as strong as opiates. Acute toxicity → hypertension, stroke, seizures,
Toxicity/S.E.s: Irritability & manic behavior (large doses). Prolonged use → cardiac arrhythmias. Very strong psych. dependence. Mild physical dependence. W/drawal
toxic psychosis (looks like paranoid schiz.). Produces psych → ↑ appetite, fatigue, depression.
Utility: Used in ENT surgery to produce local anesthesia, hemostasis, vasoconstriction. Crack =
dependence (depression on w/drawal). C/I: hyperthyroidism, mod-
smokable version.
severe hypertension, hist. of drug abuse, glaucoma, hist. of Special Features: Does not require concomitant application of a vasoconstrictor. Twice the potency
hypersens. or idiosync. to sympathomimetic amines. of procaine. Produces elevation of mood, euphoria, ↑ self-esteem, ↑ energy, ↓ sense of
Utility: Treat ADHD, narcolepsy. fatigue. Moderate dose → ↑ HR, ↑ BP.
Special Features: Not metab. by COMT. Decreased metab. by MAO.

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Name: Dextroamphetamine (Dexedrine) Name: Caffeine
Class: CNS Stimulant
Mech.: CNS Mech = Release of DA, NE, & 5HT from nerve terminals. Some Class: Xanthine
blockade of reuptake of DA, NE, & 5HT. Weak inhib. of MAO. Produces Mech.: Mobilizes Ca2+ stores. Inhibition of phosphodiesterase → ↑ cAMP.
elev. of mood, euphoria, ↑ alertness, ↓ sense of fatigue, ↓ food intake, Antagonizes adenosine receptors. Causes ↓ drowsiness, ↓ fatigue,
periph. sympathomimetic effects. faster/clearer thought flow, improved motor performance, ↓ reaction time,
Absorption: Oral → good bioavail. cardiac stim., bronchodilation, mild diuresis, gastric acid secretion.
Dist.: Crosses BBB.
Absorption:
Metab.:
Excretion, t_: Dist.:
Toxicity/S.E.s: Irritability & manic behavior (large doses). Prolonged use → Metab.:
toxic psychosis (looks like paranoid schiz.). Produces very strong Excretion, t_:
psych. dependence (depression on w/drawal), mild phys. Toxicity/S.E.s: Restlessness, insomnia, tremors, seizures, mild diuresis, cardiac
dependence. C/I: hyperthyroidism, mod-severe hypertension, hist. stim., gastric acid secretion.
of drug abuse, glaucoma, hist. of hypersens. or idiosync. to
sympathomimetic amines. Utility: OTC CNS stimulants.
Utility: Treat narcolepsy, ADHD, short term Rx of exogenous obesity. Special Features:
Special Features: Not metab. by COMT. Decreased metab. by MAO.

Name: Strychnine Name: Doxapram (Dopram)


Class: Convulsant Class: Analeptic
Mech.: Competitive glycine receptor antagonism. ↑ neuron excitability due to Mech.: Direct stim. of medullary resp. centers → stimulation of respiration. May
selective block of inhib. impulses (i.e., interf. w/recurrent Renshaw cell stim. resp. via reflex effect on periph. chemoreceptors.
inhib. at skeletal muscle motor neurons). Sim. to tetanus toxin. Absorption:
Absorption: Dist.:
Dist.: Metab.:
Metab.: Excretion, t_:
Excretion, t_:
Toxicity/S.E.s: Large doses → tonic-clonic seizures.
Toxicity/S.E.s: Tightness of neck and jaw muscles. Symm. tonic convulsions
Utility: Occasionally used to treat acute resp. failure assoc. w/COPD. Prev.
(aggravated by sensory stim.). Resp. paralysis. Impaired resp. → used to treat resp. depression assoc. w/CNS depressant overdose. No
hypoxia → medullary paralysis → death. longer recommended for this use due to high potential for seizures.
Utility: Pesticide/rodenticide. Special Features:
Special Features: Treat poisoning w/IV diazepam, insulation from sensory input,
and respiratory support.

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Name: Procaine (Novocain) Name: Benzocaine
Class: Local Anesthetic (Ester) Class: Local Anesthetic (Ester)
Mech.: Blocks Na+ & Ca2+ channels → ↓ rate of rise of action potential, failure to Mech.: Blocks Na+ & Ca2+ channels → ↓ rate of rise of action potential, failure to
propagate action potential, eventual conduction block. Smaller, propagate action potential, eventual conduction block. Smaller,
unmyelinated fibers are more easily blocked and remain blocked longer. unmyelinated fibers are more easily blocked and remain blocked longer.
Absorption: Rapidly absorbed IV & oral. IV absorption can be limited w/a Absorption: Topical use only.
vasoconstrictor. Rapid topical absorption at mucous membranes.
Dist.:
Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart).
Metab.: Rapidly metab. by plasma pseudocholinesterases. Metab.: Absorbed benzocaine is rapidly metab. by plasma
pseudocholinesterases.
Excretion, t_: Short duration of action.
Excretion, t_:
Toxicity/S.E.s: Progressive CNS effects—agitation leading to convulsions,
generalized CNS and resp. depression, CV depression, death. Toxicity/S.E.s: Too slowly absorbed to produce serious systemic toxicity..
Rare hypersens. rxns assoc. w/histamine release. Utility: Sustained anesthetic effect when applied to wounds and ulcerated
Utility: Surface anesthesia, infiltration anesth., field block anesth., nerve block surfaces.
anesth., IV regional anesth., spinal anesth., epidural anesth. Special Features:
Special Features: Rel. low potency. Sometimes used w/epinephrine to prolong
action and decrease system toxicity.

Name: Lidocaine (Xylocaine) Name: Bupivacaine (Marcaine)


Class: Local Anesthetic (Amide) Class: Local Anesthetic (Amide)
Mech.: Blocks Na+ & Ca2+ channels → ↓ rate of rise of action potential, failure to
Mech.: Blocks Na+ & Ca2+ channels → ↓ rate of rise of action potential, failure to
propagate action potential, eventual conduction block. Smaller,
propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more easily blocked and remain blocked longer.
unmyelinated fibers are more easily blocked and remain blocked longer. Absorption: Rapidly absorbed IV & oral. IV absorption can be limited w/a
Absorption: Rapidly absorbed IV & oral. IV absorption can be limited w/a vasoconstrictor. Rapid topical absorption at mucous membranes.
vasoconstrictor. Rapid topical absorption at mucous membranes. Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart).
Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart). Placental transfer inversely related to level of protein binding. 95%
Metab.: Metab. by liver microsomal enzymes. protein bound. ∴ most preferred obstetric agent.
Excretion, t_: Med. duration of action. Metab.: Metab. by liver microsomal enzymes.
Toxicity/S.E.s: Progressive CNS effects—agitation leading to convulsions, Excretion, t_: Long duration of action.
generalized CNS and resp. depression, CV depression, death. Toxicity/S.E.s: Progressive CNS effects—agitation leading to convulsions,
generalized CNS and resp. depression, CV depression, death.
Utility: Surface anesthesia, infiltration anesth., field block anesth., nerve block
Utility: Surface anesthesia, infiltration anesth., field block anesth., nerve block
anesth., IV regional anesth., spinal anesth., epidural anesth.
anesth., IV regional anesth., spinal anesth., epidural anesth.
Special Features: 4x as potent as procaine. Sometimes used w/epinephrine to Special Features: 16x as potent as procaine. Sometimes used w/epinephrine to
prolong action and decrease system toxicity. prolong action and decrease system toxicity.

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Name: Nitrous Oxide Name: Halothane (Fluothane)
Class: General Anesthetic (Anesthetic Gas) Class: General Anesthetic (Halogenated Hydrocarbon)
Mech.: Stabilizes membranes of excitable tissue → inhibition of action potential Mech.: Stabilizes membranes of excitable tissue → inhibition of action potential
(primarily pre-synaptic blockade of synaptic transmission). (primarily pre-synaptic blockade of synaptic transmission).
Absorption: Inhaled. Poor blood solubility → Rapid onset of effect (Blood/gas Absorption: Inhaled. High blood solubility→Rel. slow onset of effect (BGPC =
partition coefficient = 0.47). High conc. required for effect (MAC = 2.3). MAC = 0.77.
101). Dist.: Dissolves in blood. Organs w/high perfusion are most affected.
Dist.: Dissolves in blood. Organs w/high perfusion are most affected. Metab.: Some liver metab.
Metab.: Excretion, t_:
Excretion, t_: Primarily unmetab. excretion via lungs. Toxicity/S.E.s: High level of cardiac depression. Depresses circulation. May
Toxicity/S.E.s: Low arrhythmia potential. Low level of cardiac depression. produce fatal hepatitis. Med. high potential for arrhythmia. Avoid
Utility: Used as an adjunct to potentiate anesthesia. repeated exposure.
Special Features: Non-irritating, non-flammable. No circulatory depression. Utility: Induces general anesthesia.
Cannot be used alone to produce general anesthesia. Good Special Features: Non-irritating, non-flammable. Satisfact. analgesia and
analgesic. Poor muscle relaxant. muscle relaxation.

Name: Isoflurane (Forane) Name: Desflurane (Suprane)


Class: General Anesthetic (Halogenated Hydrocarbon) Class: General Anesthetic (Halogenated Hydrocarbon)
Mech.: Stabilizes membranes of excitable tissue → inhibition of action potential Mech.: Stabilizes membranes of excitable tissue → inhibition of action potential
(primarily pre-synaptic blockade of synaptic transmission). (primarily pre-synaptic blockade of synaptic transmission).
Absorption:Inhaled. Interm. blood solubility→Interm. onset of effect (BGPC = Absorption: Inhaled. Low blood solubility→Rapid onset of effect (BGPC = 0.42).
1.4). MAC = 1.40. MAC = 6-7.
Dist.: Dissolves in blood. Organs w/high perfusion are most affected. Dist.: Dissolves in blood. Organs w/high perfusion are most affected.
Metab.: Very little liver metab. (2%). Metab.: Some liver metab.
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: Moderately irritating. Low level of cardiac depression. Toxicity/S.E.s: Moderately irritating. Low level of cardiac depression.
Depresses circulation. Low potential for arrhythmia. Depresses circulation. Low potential for arrhythmia.
Utility: Induces general anesthesia. Utility: Induces general anesthesia.
Special Features: Lowest toxicity of the volatile liquids. Non-flammable. Special Features: Produces rapid induction/awakening. Non-flammable.
Satisfact. analgesia, good relaxation. Satisfact. analgesia, good relaxation.

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Name: Thiopental (Pentothal) Name: Midazolam (Versed)
Class: General Anesthetic (IV Induction Agent) Class: General Anesthetic (IV Induction Agent) (BZD)
Mech.: Mech.:
Absorption: IV → rapid onset of effect. Absorption: IV
Dist.: Dissolves in blood. Organs w/high perfusion are most affected. Dist.: Dissolves in blood. Organs w/high perfusion are most affected.
Metab.: Hepatic metab. Metab.:
Excretion, t_: Short duration of effect. Moderate t_.
Excretion, t_: Rapidly diffuses out of brain and redistributes to other tissues (1°
Toxicity/S.E.s: Slight CV depression. Minimal resp. depression.
terminator of action) → short duration of effect. But long t_.
Utility: Induces general anesthesia.
Toxicity/S.E.s: Dose-dependent CV depression. Mod. resp. depression.
Special Features: No analgesia. Causes high incidence of amnesia, so freq.
Utility: Induces general anesthesia. given before induction of general anesthesia.
Special Features: No analgesia. Still one of most common agents used.

Name: Propofol (Diprivan) Name: Fentanyl


Class: General Anesthetic (IV Induction Agent) Class: General Anesthetic (IV Opioid)
Mech.: Mech.:
Absorption: IV Absorption: IV
Dist.: Dissolves in blood. Organs w/high perfusion are most affected. Dist.: Dissolves in blood. Organs w/high perfusion are most affected.
Metab.: Hepatic metab. Metab.:
Excretion, t_: Short duration of effect. Short t_. Excretion, t_: Short duration of effect. Short t_.
Toxicity/S.E.s: Some CV depression. Mod. resp. depression. Toxicity/S.E.s: Slight CV depression. Resp. depression (mild-apnea).
Utility: Induces general anesthesia. Utility: Induces general anesthesia.
Special Features: No analgesia. Special Features: Excellent analgesia.

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Name: Diazepam (Valium)
Name: Ketamine (Ketalar)
Class: Antianxiety-Sedative-Hypnotic Agent (Benzodiazepine) (Antiepileptic-Status)
Class: General Anesthetic (IV Anesthetic Agent) Mech.: Acts on BZD receptors closely coupled to GABAA receptors → enhancement of GABA inhib.
Mech.: Blocks membrane effects of glutamic acid at NMDA receptors. Related to action via ↑ freq. of Cl- channel opening.
Absorption: Oral → rapid absorption (large variability in indiv. responsiveness). IV for seizures &
PCP.
conscious sedation, but may cause pain & phlebitis. IM → poor bioavailability (avoid).
Absorption: IV Dist.: Protein binding 99%. High lipid solubility. Rapid CNS dist. Accum. in fat.
Dist.: Dissolves in blood. Organs w/high perfusion are most affected. Metab.: Liver microsomal N-dealkylation/hydroxylation, then conjug → inactive glucuronides. No
induction of hepatic microsomal enzymes.
Metab.: Hepatic metab. Excretion, t_: Urine—mostly metabolized. Long—50-150 hr. Active metabolites.
Excretion, t_: Urinary & biliary excretion. Short duration of effect. Mod. t_. Toxicity/S.E.s: All dose-related. Acute—excessive depression of CNS fxns (drowsiness, sleep,
confusion, disorientation, ataxia, slurred speech, nystagmus, mild amnesia, dementia). May also
Toxicity/S.E.s: CV stimulation. Minimal resp. depression. Emergence cause aggression, hyperactivity, delirium, insomnia. Large doses or mixture w/depressants (e.g.,
phenomena include disorientation, sensory & perceptual illusions, EtOH) may cause resp. depression, coma, hallucinations, nightmares, confusion.
and vivid dreams (prior admin. of diazepam reduces incidence). Chronic—impaired thinking/memory, weight gain/loss. May exacerbate depression. Habituation &
Utility: General anesthetic. Also inducing agent. physical dependence → w/drawal syndrome. Abrupt discontinuation → risk for convulsion (but less
risk than w/newer BZDs). Symptoms have long latency (5+ days). Metab. ↓ in elderly and by
Special Features: Excellent analgesia. cimetidine. Overdose → serious resp. depression (rarely fatal w/support). Psych & phys depend.
Utility: Anxiety, insomnia, relief of alcohol w/drawal symptoms, anesthesia. Sedation—all BZDs
are DOCs for sedation. Anticonvulsant—a DOC (IV) for status epilepticus or drug-induced
seizures. Skeletal muscle relaxation—spasms, tetanus, orthopedic manipulations.

Name: Triazolam (Halcion) Name: Alprazolam (Xanax)


Class: Antianxiety-Sedative-Hypnotic Agent (Benzodiazepine) Class: Antianxiety-Sedative-Hypnotic Agent (Benzodiazepine)
Mech.: Acts on BZD receptors closely coupled to GABAA receptors → enhancement of GABA inhib. Mech.: Acts on BZD receptors closely coupled to GABAA receptors → enhancement of GABA inhib.
action via ↑ freq. of Cl- channel opening. action via ↑ freq. of Cl- channel opening.
Absorption: Oral → rapid absorption (large variability in indiv. responsiveness). Absorption: Oral → rapid absorption (large variability in indiv. responsiveness).
Dist.: Protein binding ≥50%. CNS. Dist.: Protein binding ≥50%. CNS.
Metab.: Liver microsomal N-dealkylation/hydroxylation, then conjug → inactive glucuronides. No Metab.: Liver microsomal N-dealkylation/hydroxylation, then conjug → inactive glucuronides. No
induction of hepatic microsomal enzymes. induction of hepatic microsomal enzymes.
Excretion, t_: Urine—mostly metabolized. Short—3-5 hr. Active metabolites. Excretion, t_: Urine—mostly metabolized. Short—12-15 hr. Active metabolites.
Toxicity/S.E.s: Acute—excessive depression of CNS fxns (drowsiness, sleep, confusion, Toxicity/S.E.s: Acute—excessive depression of CNS fxns (drowsiness, sleep, confusion,
disorientation, ataxia, slurred speech, nystagmus, mild amnesia, dementia). Early morning disorientation, ataxia, slurred speech, nystagmus, mild amnesia, dementia). Early morning
awakening, rebound insomnia. May also cause aggression, hyperactivity, delirium, insomnia. awakening, rebound insomnia. May also cause aggression, hyperactivity, delirium, insomnia.
Large doses or mixture w/depressants (e.g., EtOH) may cause resp. depression, coma, Large doses or mixture w/depressants (e.g., EtOH) may cause resp. depression, coma,
hallucinations, nightmares, confusion. Chronic—impaired thinking/memory, weight gain/loss. hallucinations, nightmares, confusion. Chronic—impaired thinking/memory, weight gain/loss.
Habituation & physical dependence → w/drawal syndrome. Abrupt discontinuation → risk for Habituation & physical dependence → w/drawal syndrome. Abrupt discontinuation → risk for
convulsion (greater risk than w/older BZDs). Metab. ↓ in elderly and by cimetidine. Overdose → convulsion (greater risk than w/older BZDs). Metab. ↓ in elderly and by cimetidine. Overdose
serious resp. depression (rarely fatal w/support). Psych & phys dependence. → serious resp. depression (rarely fatal w/support). Psychological and physical dependence.
Utility: Insomnia, anxiety, alcohol w/drawal. Sedation—all BZDs are DOCs for sedation. Utility: Panic/depression. Anxiety, insomnia, alcohol w/drawal. Sedation—all BZDs are DOCs for
Special Features: Newer BZD (shorter t_, greater potency). sedation.
Special Features: Newer BZD (shorter t_, greater potency).

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Name: Flurazepam (Dalmane) Name: Flumazenil (Romazicon)
Class: Antianxiety-Sedative-Hypnotic Agent (Benzodiazepine)
Mech.: Acts on BZD receptors closely coupled to GABAA receptors → enhancement of GABA inhib. Class: Benzodiazepine Antagonist
action via ↑ freq. of Cl- channel opening.
Absorption: Oral → rapid absorption (large variability in indiv. responsiveness). Mech.: Competitive antagonist for BZD receptor → antagonism of BZD CNS
Dist.: Protein binding ≥50%. CNS. effects, including respiration depression.
Metab.: Liver microsomal N-dealkylation/hydroxylation, then conjug → inactive glucuronides. No Absorption: IV
induction of hepatic microsomal enzymes.
Excretion, t_: Urine—mostly metabolized. Long—24-100 hr. Active metabolites. Dist.: CNS
Toxicity/S.E.s: Acute—excessive depression of CNS fxns (drowsiness, sleep, confusion, Metab.:
disorientation, ataxia, slurred speech, nystagmus, mild amnesia, dementia). May also cause
aggression, hyperactivity, delirium, insomnia. Large doses or mixture w/depressants (e.g., EtOH) Excretion, t_: Duration of action 1-4 hr. ∴ repeated admin. often required.
may cause resp. depression, coma, hallucinations, nightmares, confusion. Chronic—impaired Toxicity/S.E.s: Can precipitate severe abstinence synd. in BZD-dependent
thinking/memory, weight gain/loss. Habituation & physical dependence → w/drawal syndrome. patients.
Abrupt discontinuation → risk for convulsion (less risk than w/newer BZDs). Metab. ↓ in elderly
and by cimetidine. Overdose → serious resp. depression (rarely fatal w/support). ALL Utility: Treat CNS depressant effects of BZD overdose.
BZDs—Use caution w/↑ age, pregnancy, EtOH/subst. abuse, depression, driving/dangerous Special Features:
machinery, use of other CNS depressants, narcolepsy, hypersensitivity, chronic use > 1 wk- 1
month (except for epilepsy). Psych & phys dependence.
Utility: Anxiety, insomnia, alcohol w/drawal. Sedation—all BZDs are DOCs for sedation.
Special Features: Older BZD (longer t_, less potency).

Name: Buspirone (Bu Spar) Name: Phenobarbital


Class: Antianxiety-Sedative-Hypnotic Agents (Selective Antianxiety Agent) Class: Antianxiety-Sedative-Hypnotic Agent (Barbiturate) (Antiepileptic:Tonic-Clonic)
Mech.: Agonist for 5-HT 1A and D2 receptors. Mech.: Potentiates GABA transmission by interacting w/GABA receptor → ↑ duration of channel
Absorption: Oral → rapid absorption. opening. High doses → direct activation of Cl- channel → global CNS synaptic depression &
block of sustained high freq. repetitive firing..
Dist.:
Absorption:
Metab.: Extensive 1st-pass metab. (hepatic hydroxylation & dealkylation) → Dist.: 40-60% protein binding.
metabolites that may have slight activity. Metab.: Hepatic metab → inactive metabolites. Signif. induction of hepatic microsomal enzymes →
Excretion, t_: 2-4 hr. ↑ potential for drug interactions.
Toxicity/S.E.s: Wide safety margin. Dizziness, insomnia, nervousness, nausea, Excretion, t_: 46-136 hr (adults), 37-173 hr (kids).
headache, myoclonic jerks, chest pain, tinnitus, fatigue. Lower Toxicity/S.E.s: Dose-dependent depression of CNS fxn (mild sedation → sleep → coma → coma
incidence of CNS S.E.s than w/BZDs, but higher incidence of GI w/resp. depression → death), cognitive impairment, hyperactivity, ataxia, changes in sleep
S.E.s. Coadmin. w/haloperidol → ↑ serum haloperidol. W/MAO patterns. Non-dose-rel.—lethargy, ↓ attention span, osteopenia. Idiosync.—allergic
dermatitis, Stevens Johnson synd., serum sickness rxn, granulocyte suppress. Chronic use of
inhib. may cause ↑ BP. doses 2x-4x hypnotic dosage → tolerance & psych/phys. dependence. W/drawal symptoms
Utility: Short-term relief of anxiety w/o signif. sedation, drowsiness, or amnesia. include grand mal seizures and DTs and are potentially lethal.
Special Features: No synergistic/additive effect w/other antianxiety or hypnotic Utility: Alt. treatment for gen. tonic-clonic & partial seizures. Alt. treatment of status epilepticus.
agents. No CNS depression. No known potential for tolerance, Rarely used as backup to other sedative-hypnotic drugs. Suicide.
dependence, abuse, or withdrawal. May take more than a week Special Features: Long-acting agent
for anxiolytic effects to develop.

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Name: Pentobarbital Name: Chloral hydrate
Class: Antianxiety-Sedative-Hypnotic Agent (Barbiturate)
Mech.: Potentiates GABA transmission by interacting w/GABA receptor. High Class: Antianxiety-Sedative-Hypnotic Agent
doses → direct activation of Cl- channel → global CNS synaptic Mech.: Sim. to barbiturates
depression. Absorption:
Absorption: Dist.:
Dist.:
Metab.:
Metab.: Hepatic metab → inactive metabolites. Signif. induction of hepatic
Excretion, t_:
microsomal enzymes → ↑ potential for drug interactions.
Toxicity/S.E.s:
Excretion, t_:
Toxicity/S.E.s: Dose-dependent depression of CNS fxn (mild sedation → sleep Utility: Used in hospitals, nursing homes, pediatric dental settings. Mickey Finn.
→ coma → coma w/resp. depression → death). Chronic use of Special Features: Rarely used.
doses 2x-4x hypnotic dosage → tolerance & psych/phys.
dependence. W/drawal symptoms include grand mal seizures and
DTs and are potentially lethal.
Utility: Rarely used as backup to other sedative-hypnotic drugs. Suicide.
Special Features: Short-acting agent

Name: Zolpidem (Ambien) Name: Diphenhydramine (Benadryl)


Class: Antianxiety-Sedative-Hypnotic Agent Class: H1-Histamine Antagonist (OTC)
Mech.: Binds to BDZ receptors, although it’s not structurally related to BDZs. Mech.: Competitive inhib. of histamine and histamine receptor interaction.
Absorption: Absorption:
Dist.: Dist.: Enters CNS
Metab.: Excretion, t_:
Excretion, t_: Toxicity/S.E.s: Sedation (not in everyone). Taken w/alcohol → enhanced CNS
Toxicity/S.E.s: Tolerance and physical dependence rarely develop. depression. Local anesthetic activity. Acute poisoning in kids →
Utility: Short-term treatment of insomnia. As effective as BZDs in prolonging complex CNS excitatory and depressant effects (convulsions,
total sleep time and shortening sleep latency. Little effect on sleep hyperpyrexia). Topical use = highest risk of sensitization, ∴
stages. shouldn’t be applied topically.
Special Features: Utility: Treat allergic rxns (e.g., hay fever). Prevent motion sickness. Can be
used for morning sickness. Treat PD symptoms (esp. geriatric patients).
Special Features: Most effective if taken prophylactically. Can’t reverse effects
once histamine has bound to receptor. Therapeutically
effective dose related to amount of antigen.

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Name: Morphine Name: Codeine
Class: Opioid (Alkaloid) Class: Opioid (Alkaloid)
Mech.: Agonist of opioid receptors. Causes analgesia (↑ threshold for pain, ↓ subjective rxn), Mech.: Agonist of opioid receptors. Causes analgesia (↑ threshold for pain, ↓ subjective rxn),
antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression,
miosis, n/v, ↓ body temp., ↑ ACTH/PRO/GH, ↓ LH/TSH (hormone effects usu. non- miosis, n/v, ↓ body temp., ↑ ACTH/PRO/GH, ↓ LH/TSH (hormone effects usu. non-
consequential), occasionally hypotension, constipation, ↑ biliary/ureteral/bladder muscle tone, ↓ consequential), occasionally hypotension, constipation, ↑ biliary/ureteral/bladder muscle tone, ↓
uteral muscle tone, histamine release (hypotension, urticaria, itching). uteral muscle tone, histamine release (hypotension, urticaria, itching).
Absorption: IM, subcut., mucous membranes, intrathecal, oral (1st pass metab → low Absorption: IM, subcut., mucous membranes, oral (high oral:parenteral potency).
oral:parenteral potency) Metab.: Hepatic conjug. → polar metabolites.
Metab.: Hepatic conjug. → polar metabolites. Excretion, t_: Urine. Duration of analgesia—3-4 hr.
Excretion, t_: Urine. Duration of analgesia—4-5 hr. Toxicity/S.E.s: Histamine release → asthma in suscept. patients. Use w/caution w/compromised
Toxicity/S.E.s: Histamine release → asthma in suscept. patients. Use w/caution w/compromised resp. patients. CO2 retention → ↑ intracranial pressure (may mask signs of head injury).
resp. patients. CO2 retention → ↑ intracranial pressure (may mask signs of head injury). Poisoning → coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to
Poisoning → coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to 100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression.
100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. Physical dependence—abrupt w/drawal → rhinorrhea, lacrimation, chills, goose pimples,
Physical dependence—abrupt w/drawal → rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also
hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Drug interactions—sedative hypnotics → severe CNS/resp.
psychological dependence. Drug interactions—sedative hypnotics → severe CNS/resp. depression; phenothiazines/tricyclic antidepressants → ↑ sedation, freq. resp. depression.
depression; phenothiazines/tricyclic antidepressants → ↑ sedation, freq. resp. depression. Utility: Antitussant. Analgesia.
Utility: Analgesia. Intrathecal for post-surg. pain → long duration of action, few side effects. Special Features: Low maximum efficacy. Medium addiction/abuse liability. Psych. dependence.
Special Features: High maximum efficacy. High addiction/abuse liability. Psych. dependence.

Name: Heroin Name: Dextromethorphan


Class: Opioid (Semi-synthetic)
Mech.: Agonist of opioid receptors. Causes analgesia (↑ threshold for pain, ↓ subjective rxn), Class: Opioid (Semi-synthetic) (OTC)
antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, Mech.: Agonist of opioid receptors → depression of CNS cough center.
miosis, n/v, ↓ body temp., ↑ ACTH/PRO/GH, ↓ LH/TSH (hormone effects usu. non-
consequential), occasionally hypotension, constipation, ↑ biliary/ureteral/bladder muscle tone, ↓ Absorption: Oral.
uteral muscle tone, histamine release (hypotension, urticaria, itching). Init. ↓ of adenylate Metab.: Hepatic conjug. → polar metabolites.
cyclase in locus coeruleus & symp. pregang. neurons. Tolerance develops.
Absorption: IM, subcut., mucous membranes, oral, smoking. Excretion, t_: Urine.
Metab.: Hepatic conjug. → polar metabolites. Excretion, t_: Urine. Toxicity/S.E.s:High doses → hallucinations. Potentially fatal interactions with
Toxicity/S.E.s: Histamine release → asthma in suscept. patients. Use w/caution w/compromised
resp. patients. CO2 retention → ↑ intracranial pressure (may mask signs of head injury). MAOIs.
Poisoning → coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to Utility: Antitussant.
100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. Special Features: Minimal addiction/abuse liability.
Physical dependence—abrupt w/drawal (prob. med. by hyperactive adenylate cyclase) →
rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting,
diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Drug
interactions—sedative hypnotics → severe CNS/resp. depression; phenothiazines/tricyclic
antidepressants → ↑ sedation, freq. resp. depression.
Special Features: High addiction/abuse liability. Psych. dependence.

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Name: Methadone (Dolophine) Name: Meperidine (Demerol)
Class: Opioid (Synthetic-Analgesic) (Withdrawal Suppressant) Class: Opioid (Synthetic-Analgesic)
Mech.: Agonist of opioid receptors. Causes analgesia (↑ threshold for pain, ↓ subjective rxn), Mech.: Agonist of opioid receptors. Causes analgesia (↑ threshold for pain, ↓ subjective rxn),
antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression,
miosis, n/v, ↓ body temp., ↑ ACTH/PRO/GH, ↓ LH/TSH (hormone effects usu. non- miosis, n/v, ↓ body temp., ↑ ACTH/PRO/GH, ↓ LH/TSH (hormone effects usu. non-
consequential), occasionally hypotension, constipation, ↑ biliary/ureteral/bladder muscle tone, ↓ consequential), occasionally hypotension, constipation, ↑ biliary/ureteral/bladder muscle tone, ↓
uteral muscle tone, histamine release (hypotension, urticaria, itching). uteral muscle tone, histamine release (hypotension, urticaria, itching).
Absorption: IM, subcut., oral (high oral:parenteral potency). Absorp.: IM, subcut., oral (1st pass metab → med. oral:parenteral potency).
Metab.: Hepatic conjug. → polar metabolites. Metab.: Hepatic conjug.→polar metabolites. Excretion, t_: Urine. Duration of analgesia—2-4 hr.
Excretion, t_: Urine. Duration of analgesia—4-6 hr. Toxicity/S.E.s: Histamine release → asthma in suscept. patients. Use w/caution w/compromised
Toxicity/S.E.s: Histamine release → asthma in suscept. patients. Use w/caution w/compromised resp. patients. CO2 retention → ↑ intracranial pressure (may mask signs of head injury).
resp. patients. CO2 retention → ↑ intracranial pressure (may mask signs of head injury). Poisoning → coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to
Poisoning → coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to 100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression.
100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. Physical dependence—abrupt w/drawal → rhinorrhea, lacrimation, chills, goose pimples,
Physical dependence—abrupt w/drawal → rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also
hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Drug interactions—sedative hypnotics → severe CNS/resp.
psychological dependence. Drug interactions—sedative hypnotics → severe CNS/resp. depression; phenothiazines/tricyclic antidepressants → ↑ sedation, freq. resp. depression; MAO
depression; phenothiazines/tricyclic antidepressants → ↑ sedation, freq. resp. depression. inhib → hyperpyrexia, coma, convulsions.
Utility: Treatment of physical dependence to other opioids, esp. heroin (less severe w/drawal Utility: Analgesia.
synd.). Analgesia. Migraine relief. Special Features: High maximum efficacy. High addiction/abuse liability. Psych. dependence.Less
Special Features: High maximum efficacy. High addiction/abuse liability. Psych. dependence. severe constipation, effect on smooth muscle. Less predictable miosis.

Name: Propoxyphene (Darvon) Name: Pentazocine (Talwin)


Class: Opioid (Synthetic-Analgesic) Class: Opioid (Synthetic-Analgesic)
Mech.: Agonist of opioid receptors. Causes analgesia (↑ threshold for pain, ↓ subjective rxn),
antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, Mech.: Mixed agonist-antagonist of opioid receptors. Causes analgesia (↑
miosis, n/v, ↓ body temp., ↑ ACTH/PRO/GH, ↓ LH/TSH (hormone effects usu. non- threshold for pain, ↓ subjective rxn), sedation, resp. depression.
consequential), occasionally hypotension, constipation, ↑ biliary/ureteral/bladder muscle tone, ↓ Absorption: IM, subcut, oral (1st pass metab → med. oral:parenteral potency).
uteral muscle tone, histamine release (hypotension, urticaria, itching).
Absorption: Oral Metab.: Hepatic conjug.→polar metabolites. Excretion, t_: Urine. Duration of
Metab.: Hepatic conjug. → polar metabolites. analgesia—3-4 hr.
Excretion, t_: Urine. Duration of analgesia—4-5 hr. Toxicity/S.E.s: CO2 retention → ↑ intracranial pressure (may mask signs of head
Toxicity/S.E.s: Histamine release → asthma in suscept. patients. Use w/caution w/compromised
resp. patients. CO2 retention → ↑ intracranial pressure (may mask signs of head injury). injury). Tolerance (up to 100x) to analgesia, sedation, resp. depression.
Poisoning → coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to Physical dependence—abrupt w/drawal → rhinorrhea, lacrimation, chills, goose
100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety,
Physical dependence—abrupt w/drawal → rhinorrhea, lacrimation, chills, goose pimples, hostility (but it’s not fatal). Also psychological dependence. Precipitates
hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also
psychological dependence. Drug interactions—sedative hypnotics → severe CNS/resp. w/drawal synd. Large doses → dysphoria & hallucinations. Drug
depression; phenothiazines/tricyclic antidepressants → ↑ sedation, freq. resp. depression. interactions—sedative hypnotics → severe CNS/resp. depression;
Utility: Limited analgesia (no more than aspirin in usu. therapeutic dose, but augments the effects of
aspirin & acetaminophen. phenothiazines/tricyclic antidepressants → ↑ sedation, freq. resp. depression.
Special Features: Very low maximum efficacy (limited analgesia). Low addiction/abuse liability. Utility: Analgesia. Orig. thought to lack abuse liability.
Special Features: Mod. maximum efficacy. Low addiction/abuse liability.
Psych. dependence.

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Name: Fentanyl (Innovar) Name: Tramadol (Ultram)
Class: Opioid (Synthetic-Analgesic) Class: Opioid (Synthetic-Analgesic)
Mech.: Agonist of opioid receptors. Causes analgesia (↑ threshold for pain, ↓ subjective rxn), Mech: Low affinity binding of tramadol to mu-opioid receptors and higher affinity
antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, binding of the M1 metabolite. Opioid effects only partially antagonized by
miosis, n/v, ↓ body temp., ↑ ACTH/PRO/GH, ↓ LH/TSH (hormone effects usu. non-
consequential), occasionally hypotension, constipation, ↑ biliary/ureteral/bladder muscle tone, ↓ naloxone. Also inhibits reuptake of norepinephrine and serotonin.
uteral muscle tone, histamine release (hypotension, urticaria, itching). Absorption:
Absorption: Parenteral, transdermal patch, lollipop. Metab:
Metab.: Hepatic conjug. → polar metabolites. Excretion, t_:
Excretion, t_: Urine. Duration of analgesia—1-1.5 hr. Toxicity/S.E.s: Sim. to opioids—dizziness, somnolence, nausea, constipation,
Toxicity/S.E.s: Histamine release → asthma in suscept. patients. Use w/caution w/compromised sweating, & pruritus. Unlike opioids, significantly less respiratory
resp. patients. CO2 retention → ↑ intracranial pressure (may mask signs of head injury). depression, no histamine release. At therapeutic doses, no effect on
Poisoning → coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to heart rate, left-ventricular function, or cardiac index. Some orthostatic
100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. hypotension. Seizures. Use w/caution w/CNS depressants, MAO
Physical dependence—abrupt w/drawal → rhinorrhea, lacrimation, chills, goose pimples,
hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also inhibitors. May trigger opioid w/drawal symptoms.
psychological dependence. Drug interactions—sedative hypnotics → severe CNS/resp. Utility: Analgesia.
depression; phenothiazines/tricyclic antidepressants → ↑ sedation, freq. resp. depression. Special Features: Inhib. reuptake of NE and 5HT.
Utility: Analgesia. Induction of general anesthesia.
Special Features: Very high maximum efficacy. High addiction/abuse liability. Psych. dependence.

Name: Loperamide (Imodium) Name: Diphenoxylate-Atropine (Lomotil)


Class: Opioid (Antidiarrheal) (OTC) Class: Opioid (Antidiarrheal)
Mech.: Increased gastric tone → delayed gastric emptying. Increase tone and Mech.: Increased gastric tone → delayed gastric emptying. ↑ tone and ↓
decreasesd propulsive peristaltic waves in large intest. → decreased gut propulsive peristaltic waves in large intest. → ↓ gut motility. Effects due
motility. Effects due to inhib. of ACh release by neurons in the intest. to inhib. of ACh release by neurons in the intest. wall. Naloxone sensitive.
wall. Naloxone sensitive. Anti-secretory effect (non-naloxone Absorption: Oral
sensitive). Dist.:
Absorption: Oral Metab.:
Excretion, t_:
Dist.: 90% → GI tract and liver. Very little CNS.
Toxicity/S.E.s: Recommended dose → dizziness, drowsiness, mild euphoria.
Metab.:
Excessive doses → pronounced euphoria, potentially serious respiratory
Excretion, t_:
depression (may not be evident until 12-30 hr later). ↓ peristalsis → ↓
Toxicity/S.E.s: ↓ peristalsis → ↓ evacuation of bacteria and toxins. evacuation of bacteria and toxins. Use w/great caution in kids. Potentiates
Utility: Antidiarrheal. effects of barbiturate, tranquilizers, alcohol, other narcotics. Hypertensive
crisis w/MAOI.
Special Features: No abuse liability. Preferred anti-diarrheal of the opioids.
Less potential for analgesia, respiratory depression, and addiction than other Utility: Antidiarrheal.
opioids. Much safer than other opioids. Longer lasting effects than Special Features:
dephnoxylate.

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Name: Naloxone (Narcan) Name: Naltrexone (Trexan)
Class: Opioid Antagonist Class: Opioid Antagonist
Mech.: Competitive inhib. at opioid receptors. Mech.: Competitive inhib. at opioid receptors.
Absorption: IV Absorption: Oral
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Duration of action ~ 1 hr. Excretion, t_: Long duration of action.
Toxicity/S.E.s: Toxicity/S.E.s:
Utility: Treat opioid poisoning. Utility: “Maintenance” drug for opioid addicts in rehab. programs. May also
Special Features: May require intermittent dosing, as half life is so short. decrease alcohol craving in chronic alcoholics.
Special Features:

Name: Clonidine (Catapres) Name: Sumatriptan (Imitrex)


Class: Anti-Migraine (Serotonin Agonist)
Class: Centrally Acting Antiadrenergic Agent/Opioid Withdrawal Suppressant
Mech.: Stim 5-HT1D receptors → cranial vasoconstriction → ↑ resistance in
Mech.: Stim. inhib. α2 receptors in central cardiovasc pathways involving EPI or carotid arteriovenous anastomoses and shunts w/minor effects on
NE. α2 are G-protein coupled to inhibit adenylyl cyclase → systemic and coronary artery vasculature.
↓ cAMP → ↓ central symp. activity. Absorption: Subcut. (96% bioavailability) → peak plasma conc. in 5-20 min.
Response in 10-30 min; 10-13 hour duration. Oral (14%
Absorption:
bioavailability) → clinical response in 30-60 min.
Dist.: Act at medullary and spinal sites.
Dist.:
Metab.: Metab.: 80% metab.
Excretion, t_: Excretion, t_: 2 hr.
Toxicity/S.E.s: Prominent sedation, dry mouth. Toxicity/S.E.s: Pain, swelling, redness at injection site. Feeling of heaviness,
tightness in chest (injection). Neuro symptoms (tingling,
Utility: Treat hypertension. DOC for treating opioid w/drawal (probably warm/burning sensation). Rare vasospasm in patients w/coronary
substitutes for opioid depression of adenylate cyclase in locus coeruleus
artery disease (→ angina, MI). 34-46% headaches recur in 24-48
& pregang. symp. neurons. No abstinence synd. when withdrawn.
hr.
Special Features: Direct α2 activation. Very potent (<0.5 mg/day). Utility: Partial/complete relief of migraine headache in 80% w/in 2 hr (subcut).
Relieves n/v, photophobia, phonophobia.
Special Features: Oral effective, w/few side effects at lowest doses.
Expensive.

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Name: Ergotamine Name: Dihydroergotamine
Class: Anti-Migraine (Serotonin Agonist) Class: Anti-Migraine (Serotonin Agonist)
Mech.: Partial agony at 5-HT2 vascular receptors & partial agonist at α- Mech.: Partial agony at 5-HT2 vascular receptors & partial agonist at α-
adrenergic receptors (can act as a blocker) → vasoconstriction (cerebral adrenergic receptors (can act as a blocker) → vasoconstriction (cerebral
vasc. most sensitive), uterine smooth muscle contraction, n/v, diarrhea. vasc. most sensitive), uterine smooth muscle contraction, n/v, diarrhea.
Absorption: IV, IM, oral, sublingual, rectal, & inhaler. Absorption: IV. Investigational use intranasally & orally.
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: Most common = GI (n/v, diarrhea). Most dangerous = Toxicity/S.E.s: Most common = GI (n/v, diarrhea). Most dangerous =
vasospasm from overuse/overdose (intense & prolonged, but can vasospasm from overuse/overdose (intense & prolonged, but can
be blocked w/α blockers). Drowsiness. be blocked w/α blockers). Drowsiness.
Utility: Treat migraines. Utility: Treat migraines.
Special Features: Most effective when given during prodrome period. Often Special Features: Lower direct smooth muscle, vasospasm, and serotonin
combined w/caffeine to facilitate absorption. effects and more selective α receptor blockade than
ergotamine.

Name: Methysergide (Sansert) Other Migraine Drugs


Class: Anti-Migraine (Serotonin Agonist)
Mech.: Partial agony at 5-HT2 vascular receptors & partial agonist at α-adrenergic β Blockers: Propanolol, timolol, nadolol, metoprolol for continuous prophylaxis.
receptors (can act as a blocker) → vasoconstriction (cerebral vasc. most S.E.s include fatigue, depression, orthostatic hypotension.
sensitive), uterine smooth muscle contraction, n/v, diarrhea. C/I in asthmatics & congestive heart failure patients.
Absorption:
Dist.:
Ca2+ Channel Blockers: Verapamil & flunarazine → moderatey efficacious
Metab.:
Excretion, t_: prophylaxis.
Toxicity/S.E.s: Weight gain, peripheral edema, fibrosis (retroperitoneal,
pleuropericardial, subendocardial). Concurrent use of ergot alkaloids, β Analgesics: Fiorinal: aspirin + caffeine + butalbital. Midrin: acetaminophen +
adrenergic blockers, erythromycin, or dopamine → ↑ risk of arterial spasm isometheptene (sympathomimetic) + dichloralphenazone (sedative).
& occlusion. Occasional central stim. & hallucinations. NSAIDS, esp. naproxen sodium (but ↓ gastric motility during acute
Utility: Migraine prevention. Reserved for recurrent, refractory, severe migraine, attack may interfere w/absorption). Butorphanol (opioid agonist
as fibrosis is assoc. w/prolonged use. antagonist) nasal spray. Methadone (IM).
Special Features: Relatively ineffective in treatment of impending/active Overuse may cause a headache (“analgesic rebound”).
migraines. Useful as a prophylactic.

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Name: Phenytoin (Dilantin) Name: Carbamazepine (Tegretol)
Class: Antiepileptic Agent (Tonic-Clonic/Complex-Partial) Class: Antiepileptic Agent (Tonic-Clonic/Complex-Partial)
Mech.: Blocks voltage-dependent Na+ channels → inhib. of sustained high-freq Mech.: Blocks voltage-dependent Na+ channels → inhib. of sustained high-freq
repetitive neuron firing. repetitive neuron firing.
Absorption: Absorption:
Dist.: 69-96% protein binding. Dist.: 66-89% protein binding.
Metab.: Metab.:
Excretion, t_: 10-34 hr (adults), 5-140 hr (kids). Excretion, t_: 14-27 hr (adults), 8-28 hr (kids)
Toxicity/S.E.s: Dose-related—nystagmus, cognitive impairment, incoordination, Toxicity/S.E.s: Dose-related—double vision, blurred vision, vertigo, cognitive
dyskinesias, seizure exacerbation. Non-dose-related—hirsutism, impairment, lethargy, behavioral changes, dyskinesias, cardiac condxn
coarsening of facial features, exacerbation of acne, gingival hyperplasia, disturbances. Non-dose-rel.—diarrhea, fluid retention.
osteopenia, neuropathy, folate deficiency anemia. Idiosync.—allergic Idiosync.—granulocyte suppression, allergic dermatitis, Stevens-Johnson
dermatitis, fetal drug effects, hepatic failure, serum sickness rxn, SLE-like synd., aplastic anemia, hepatic & kidney failure. Signif. drug interactions
rxn, hyperglycemia, aplastic anemia, granulocyte suppression. Drug (↓ w/phenobarbital, phenytoin, primidone, felbamate).
interactions (↑ w/carbamazepine, felbamate; ↓ w/valproic acid). Utility: A DOC for generalized tonic-clonic seizures. A DOC for 1° & 2°
Utility: A DOC for generalized tonic-clonic seizures. A DOC for 1° & 2° generalized partial and complex-partial seizures. Treatment of pain assoc.
generalized partial and complex-partial seizures. w/true trigeminal neuralgia (off-label). Management of acute mania and
Special Features: maintenance of bipolar affective disorder (off-label).

Name: Valproate (Depakote, Depakene) Name: Ethosuximide (Zarontin)


Class: Antiepileptic Agent (Absence/Tonic-Clonic/Complex-Partial)
Class: Antiepileptic Agent (Absence)
Mech.: Multiple. Reduces T-channel Ca2+ currents → ↑ seizure threshold. May
enhance GABAergic neurotransmission. Inhib. sustained high freq. Mech.: Reduces T-channel Ca2+ currents → ↑ seizure threshold.
repetitive neuron firing. Absorption:
Dist.: 80-95% protein binding.
Dist.: 0% protein binding.
Excretion, t_: 6-15 hr (adults), 8-15 hr (kids).
Toxicity/S.E.s: Dose-rel.—GI upset, ↑ liver enzymes, tremor, hyperammonemia, Metab.:
initial somnolence, behavioral changes. Non-dose-rel.—weight gain, Excretion, t_: 20-60 hr (adults & kids)
nausea, hair loss, changes in hair texture. Idiosync.—Reye-like synd,. Toxicity/S.E.s: Dose-related—anorexia, nausea, fatigue, headache. Non-dose-
fetal drug effects, hepatic failure (esp. kids <2 y.o. on mult. drug therapy), rel.—blood-dyscrasia, SLE-like rxn, hepatitis.
pancreatitis, coma, stupor. Drug interactions (↓ w/carbamazepine, Utility: A DOC for uncomplicated absence.
phenobarbital, phenytoin; ↑ w/felbamate). Special Features:
Utility: A DOC for uncomp. gen. absence. A DOC for gen. tonic-clonic seizures.
DOC for atypical absence, myoclonic & atonic epilepsy. Treat 1° & 2°
gen. partial & complex-partial seizures. Treatment of bipolar disorder and
mgt. of aggression or violence (off-label).
Special Features:

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Name: Clonazepam (Clonopin) Name: Felbamate (Felbatol)
Class: Benzodiazepine (Antiepileptic: Absence) Class: Antiepileptic Agent (Complex-Partial)
Mech.: Acts on BZD receptors closely coupled to GABAA receptors → Mech.: Multiple. Blocks voltage-dependent Na+ channels → inhib. of sustained
enhancement of GABA inhib. action via ↑ freq. of Cl- channel opening. high-freq repetitive neuron firing. Modulates strychnine-insens. glycine
Absorption: receptor. May enhance GABAergic neurotransmission.
Dist.: Metab.: Excretion, t_: Absorption: Oral → 100% bioavail.
Toxicity/S.E.s: All dose-related. Acute—excessive depression of CNS fxns Dist.: 22-25% protein binding
(drowsiness, sleep, confusion, disorientation, ataxia, slurred speech, Metab.: 50% hepatic, 50% renal. Excretion, t_: 20-23 hr (adults)
nystagmus, mild amnesia, dementia). May also cause aggression, Toxicity/S.E.s: Most serious—aplastic anemia, acute hepatic failure. Patients &
hyperactivity, delirium, insomnia. Large doses or mixture w/depressants (e.g., physicians both required by FDA to sign info/consent form. Most
EtOH) may cause resp. depression, coma, hallucinations, nightmares, common—anorexia, n/v, insomnia, headache. Drug interactions—↓
confusion. Chronic—impaired thinking/memory, weight gain/loss. Habituation & w/phenytoin, carbamazepine.
physical dependence → w/drawal syndrome. Abrupt discontinuation → risk for Utility: Not DOC for anything. Monotherapy or adj. therapy of partial seizures in
convulsion. Metab. ↓ in elderly and by cimetidine. Overdose → serious resp. patients ≥ 14 y.o. Adj. therapy of partial & gen. seizures assoc.
depression (rarely fatal w/support). Development of tolerance. w/Lennox-Gastaut synd.
Utility: Alt. to ethosuximide and valproate for uncomp. absence. Alt. to Special Features: Broad-spectrum anticonvulsant. Effective as add-on &
valproate for atypical absence. Limited use due to development of monotherapy. But multiple drug interactions, signif. S.E.s w/initial dosing, &
tolerance. increased risk of aplastic anemia & acute hepatic failure diminish its charm.
Special Features:

Name: Gabapentin (Neurontin) Name: Lamotrigine (Lamictal)


Class: Antiepileptic Agent (Complex-Partial) Class: Antiepileptic Agent (Complex-Partial)
Mech.: Inhib. release of glutamate. Inhib Na+ -med. sustained firing.
Mech.: Unknown. Transp. into brain. Binds to unique specific receptor. Appears
Absorption: Oral → 100% bioavailability.
to inhib Na+ -med. sustained firing. ↑ brain GABA levels.
Dist.: Protein binding 55%
Absorption: Oral → 60% bioavailability. Actively absorbed by l-amino acid Metab.: Primarily hepatic metab.
transport system. Dose-dependent decrease in absorption at doses > 600 Excretion, t_: Long t_.
mg. Toxicity/S.E.s: Most common—somnolence, dizziness, headache, blurred
Dist.: <10% protein binding. vision, diplopia, ataxia, n/v. Less common—rash (mild-severe), esp.
Metab.: w/concurrent use of valproic acid. Drug interactions—↓ w/phenytoin,
Excret. t_: Almost 100% excret. unchanged by kidney (∝ to creatinine carbamazepine; ↑ w/valproic acid. ∴ When administering w/valproic acid,
clearance). 5-7 hr (adults). start w/low dose (25 mg/d), then titrate up.
Utility: Adj. therapy of partial seizures, including secondarily generalized.
Toxicity/S.E.s: Somnolence, dizziness, ataxia, fatigue, nystagmus, headache, Possible alt. for generalized absence.
tremor, diplopia, n/v. No drug interactions. Special Features: Long t_, low toxicity profile, defined therapeutic range,
Utility: Adj. therapy of partial seizures, including secondarily generalized. different mech. of action. But metab. affected by concurrent antiepileptic
Management of neuropathic pain (off-label). therapy, and experience w/monotherapy is limited.
Special Features: Cleanest (regarding drug interactions) antiepileptic drug. Low
toxicity profile. However, there is limited clinical experience w/it against
other seizure types, limited experience w/monotherapy, and it has a short t_.

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Name: L-Dopa Name: Bromocriptine (Parlodel)
Class: Antiparkinsonian Agent (Precursor) Class: Antiparkinsonian Agent (DA agonist)
Mech.: Inactive. Converted to dopamine in the brain by L-aromatic acid decarboxylase. Mech.: Full agonist at D2 receptors, partial agonist at D1 receptors.
Absorption: Oral. Absorbed from small intest. via non-specific AA transport system. Absorption Absorption:
slowed if other AAs present (i.e., if taken w/food).
Dist.: Dist.:
Metab.: MAO-B, COMT Excretion, t_: Metab.:
T/S.E.s: Wearing off—decreased length of effect. Each dose effective for only 1-2 hr., followed by Excretion, t_: 3-7 hr.
rapid return of motor deficits. Possibly controllable w/↑ dose & frequency of dosing. Toxicity/S.E.s: High incidence. Dyskinesias, orthostatic hypotension,
Dyskinesias—excessive & abnormal involuntary movements (dystonia, esp. upon waking w/low hallucinations, confusion, psychosis (C/I w/history of psychosis),
plasma levels; choreiform dyskinesia occurs during peak levels). On/off phenom.—In late PD, anorexia, n/v, cardiac arrhythmias, (C/I w/recent MI), painless
patient rapidly fluctuates btwn. having no beneficial effect from L-Dopa to having good mobility (but digital vasospasm (avoid w/periph. vascular disease).
often w/signif. dyskinesia). Others—hallucinations & confusion (clozapine may help), cardiac Utility: Relieve symptoms of Parkinson’s Disease. Reduce on/off fluctuations
arrhythmias (rare), life-threatening hypertension & pyrexia if coadmin. w/non-specific MAO and induce on/off effect less frequently.
inhibitor, may exacerbate/ppt. melanoma in predisposed patients. C/I w/closed-angle glaucoma.
Vit. B6 may ↓ efficacy. Features: Longer duration of action than L-Dopa. Doesn’t depend on residual
Utility: Treat Parkinson’s Disease symptoms. May initially produce complete improvement in dopamine neurons. ∴ May be more useful in late PD. May be as
rigidity, bradykinesia, & tremor. effective as L-Dopa in patients that respond well to L-Dopa, but patients
Features: Must be admin. w/a peripheral decarboxylase inhibitor—carbidopa (carbidopa/L-Dopa = unresponsive to L-Dopa are poor candidates for bromocriptine treatment.
Sinemet), benserazide.

Name: Pergolide (Permax) Name: Selegiline (Deprenyl, Eldepryl)


Class: Antiparkinsonian Agent (DA agonist) Class: Antiparkinsonian agent (MAO-B Inhibitor)
Mech.: Full agonist at D1 & D2 receptors. Mech.: Low doses → selective inhibition of MAO-B → prolonged action of
Absorption: endogenous DA and L-Dopa effects.
Dist.: Absorption:
Metab.: Dist.:
Excretion, t_: 3-7 hr. Metab.:
Toxicity/S.E.s: Dyskinesias, orthostatic hypotension, hallucinations, confusion, Excretion, t_:
psychosis (C/I w/history of psychosis), anorexia, n/v, cardiac Toxicity/S.E.s: Mild wearing off & on/off phenomena. However, long-term use
arrhythmias, (C/I w/recent MI), painless digital vasospasm (avoid
may → shorter time to develop adverse responses to L-Dopa. In late PD,
w/periph. vascular disease).
coadmin. w/L-Dopa may → exacerbation of adverse L-Dopa effects. C/I in
Utility: Relieve symptoms of Parkinson’s Disease. Reduce on/off fluctuations
and induce on/off effect less frequently. patients taking meperidine (→ stupor, rigidity, agitation, hyperthermia).
Features: Longer duration of action than L-Dopa. Doesn’t depend on residual Utility: Relieves symptoms of Parkinson’s Disease.
dopamine neurons. ∴ May be more useful in late PD. Special Features: Doesn’t diminish freq. of late PD problems nor postpone their
development.

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Name: Trihexyphenidyl (Artane) Name: Amantadine (Symmetrel)
Class: Antiparkinsonian Agent (Anticholinergic) Class: Antiviral/Antiparkinsonian Agent
Mech.: Blocks a late stage in assembly of influenza A virus
Mech.: Antagonizes muscarinic receptors, somehow producing alleviating
Absorption: Well absorbed orally.
effects.
Distribution:
Absorption: Oral Metab.:
Dist.: Excretion, t_: Excreted unchanged in urine.
Metab.: Toxicity/S.E.s: CNS toxicity (nervousness, confusion, hallucinations, insomnia,
Excretion, t_: Duration of action 6-12 hr. depression, confusion). Overdose → toxic psychosis. Freq. livedo
Toxicity/S.E.s: reticularis (skin mottling). Peripheral edema, freq. nausea. C/I w/hist. of
seizures or congestive heart failure. Amantadine>rimantadine
Utility: Relieves symptoms of Parkinson’s Disease. May be esp. useful in
treating prominent tremor & early morning dystonia. Little effect on Utility: Treat influenza A. Treat Parkinson’s Disease symptoms → improvement
bradykinesia. Useful in treatment of Parkinsonian syndromes produced by of akinesia, rigidity, tremor, gait disturbances, & total disability in ~ 50%
antipsychotic medications. of patients (mech. unknown). Use alone or w/L-Dopa for PD.
Special Features: Benefit is often short-lived (3-4 months). 20-30% symptomatic Features: Can be used prophylactically for influenza A. For PD, sustained
improvement in 50-75% of patients. improvement may last up to 30 months, but may also be short lived (1-3
months). For PD, as good as or better than anticholinergics.

Name: Tolcapone Name: Entacapone


Class: Antiparkinsonian (COMT Inhibitor) Class: Antiparkinsonian (COMT Inhibitor)
Mech.: Inhib. COMT → ↑ plasma conc. of L-Dopa → ↑ free L-Dopa in brain → ↑ Mech.: Inhib. COMT → ↑ plasma conc. of L-Dopa → ↑ free L-Dopa in brain → ↑
DA in brain. DA in brain.
Absorption: Absorption:
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: Nausea (from ↑ peripheral DA), ↑ dyskinesia. Toxicity/S.E.s: Nausea (from ↑ peripheral DA), ↑ dyskinesia.
Utility: Treat symptoms of Parkinson’s Disease. Increases duration of response Utility: Treat symptoms of Parkinson’s Disease. Increases duration of response
to L-Dopa, decreases required daily dose of L-Dopa. to L-Dopa, decreases required daily dose of L-Dopa.
Special Features: Special Features:

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Name: Baclofen (Lioresal) Name: Dantrolene (Dantrium)
Class: Muscle Relaxant (Centrally Acting) Class: Muscle Relaxant (Peripherally Acting)
Mech.: GABAB agonist → inhib. of neurotrans. release → ↓ release of glutamate Mech.: Decreases excitation-contraction coupling in muscle fibers by interfering
from Ia afferents & upper motor neurons. w/release of Ca2+ from sarcoplasmic reticulum.
Absorption: Absorption:
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:

Toxicity/S.E.s: Sedation (much less than diazepam), ↑ seizure activity in Toxicity/S.E.s: Muscle weakness, sedation. Chronic treatment occasionally →
epileptics, dizziness, blurred vision, muscle weakness, ataxia. hepatitis.
Utility: Preferred drug for treatment of spasticity assoc. w/ALS, spinal cord Utility: Treat spasticity due to spinal cord injury, cerebral palsy, multiple
trauma, multiple sclerosis, & cerebral palsy. sclerosis, stroke, amyotrophic lateral sclerosis. Treat malignant
hyperthermia. Treat neuroleptic malignant syndrome (efficacy prob. not
Special Features: due to block of Ca2+ release).
Special Features: A hydantoin derivative.

Name: Chlorpromazine (Thorazine) Name: Haloperidol (Haldol)


Class: Psychopharmacological Agents (Antipsychotic) (Aliphatic Phenothiazine Derivative) Class: Psychopharmacological Agents (Antipsychotic) (Butyrophenone Derivative)
Mech.: Blocks DA (esp. in limbic areas, CTZ, GI), muscarinic, α-adrenergic, H1 histaminic, & 5- Mech.: Blocks DA (esp. in limbic areas), muscarinic, α-adrenergic, H1 histaminic, & 5-HT2
HT2 receptors. receptors.
Absorption: Oral, suppository (emesis) Dist.: Metab.: Excretion, t_: Absorption: Dist.: Metab.: Excretion, t_:
Toxicity/S.E.s: Early onset extrapyramidal disorders—pseudo-Parkinsonism, akathisia, acute Toxicity/S.E.s: High incidence of extrapyramidal toxicity. Early onset extrapyramidal
dystonias (dosage reduction or anticholinergics help). Late onset extrapyram. disorder—tardive disorders—pseudo-Parkinsonism, akathisia, acute dystonias (dosage reduction or
dyskinesia (can be irreversible). Hyperprolactinemia, amenorrhea, infertility. Antimuscarinic anticholinergics help). Late onset extrapyram. disorder—tardive dyskinesia (can be
effects. Orthostatic hypotension, impotence (α). Sedation (H1). Weight gain. Allergic irreversible). Hyperprolactinemia, amenorrhea, infertility. Antimuscarinic effects. Orthostatic
agranulocytosis. Neuroleptic malignant synd.—hyperpyrexia, catatonia, excessive muscle hypotension, impotence (α). Sedation (H1). Weight gain. Allergic agranulocytosis (esp.
rigidity, altered mental status, ANS instability; incidence 1%, mortality 15%. For NMS stop Rx, w/clozapine (1-2%)). Neuroleptic malignant synd.—hyperpyrexia, catatonia, excessive muscle
admin. dantrolene (muscle relaxant) & dopamine agonists (e.g., bromocriptine). Drug rigidity, altered mental status, ANS instability; incidence 1%, mortality 15%. For NMS stop Rx,
interactions—may potentiate actions of other CNS depressants. admin. dantrolene (muscle relaxant) & dopamine agonists (e.g., bromocriptine). Drug
Utility: Treat schizophrenia, manic episodes, intractable hiccough. Treat emesis from drugs, interactions—may potentiate actions of other CNS depressants.
radiation, uremia, pain, post-op, emotional, GI irritation, cancer chemotherapy. Utility: Treat schizophrenia, Tourette’s syndrome, manic episodes, intractable hiccough, emesis.
Preanesthetic. Preanesthetic.
Features: Drug holidays important to reduce tendency for tardive dyskinesia and test for continued Features: Drug holidays important to reduce tendency for tardive dyskinesia and test for continued
need. Big problem w/non-compliance. Limit doses to min. side effects. No potential for need. Big problem w/non-compliance. Limit doses to min. side effects.
abuse.

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Name: Clozapine (Clozaril) Name: Imipramine (Tofranil)
Class: Psychopharmacological Agents (Tricyclic Antidepressant)
Class: Psychopharmacological Agents (Antipsychotic) (Dibenzodiazepine Deriv.) Mech.: Blocks NE and 5HT uptake. Also prominent muscarinic blockade.
Mech.: Blocks 5HT2, H1, α receptors. High D1 affinity, relatively low D2 affinity. Possible mechs include down-reg. of brain α2 and 5HT2 receptors or
Also acts on muscarinic and histaminic receptors. decreased number of β brain receptors.
Absorption: Absorption: Dist.: Metab.:
Dist.: Excretion, t_:
Toxicity/S.E.s: Sedation, postural hypotension, excess sweating, marked
Metab.:
decrease in REM sleep. Block antihypertensive effects of guanethidine.
Excretion, t_: Enhance effects of some sympathomimetics. Can be extremely toxic when
Toxicity/S.E.s: Sedation, seizures, antimuscarinic, activity, agranulocytosis combined w/MAO inhibs (but can also be done safely). Potentiates effects
(bone marrow toxicity). Close monitoring required (i.e., blood tests every of alcohol and other CNS depressants. Overdoses → coma, seizures,
couple of weeks). Drug interactions—w/some BZDs may cause death. hypotension, depressed resp., arrhythmias.
Utility: Treat schizophrenia, esp. patients w/tardive dyskinesia. Utility: Treat endogenous depression, enuresis, chronic pain, panic rxns, phobic
Special Features: Little, if any, tendency for extrapyramidal disorders. May anxiety.
even reverse them. More effective than other antipsychotics in Special Features: TCAs preferred over MAOIs for initial treatment of endogenous
relieving neg. symptoms of schizophrenia. depression. Severely depressed patients should never be
given more than a 1 week supply of a TCA (danger of
overdose).

Name: Amitryptiline (Elavil) Name: Phenelzine (Nardil)


Class: Psychopharmacological Agents (Tricyclic Antidepressant)
Mech.: Blocks NE and 5HT uptake. Also prominent muscarinic blockade. Class: Psychopharmacological Agents (Antidepressant) (MAOI) (Hydrazine
Deriv.)
Possible mechs include down-reg. of brain α2 and 5HT2 receptors or
decreased number of β brain receptors. Mech.: Inhib. of MAO → central build-up of NE, 5HT, DA.
Absorption: Dist.: Metab.: Absorption:
Excretion, t_: Dist.:
Toxicity/S.E.s: Prominent sedation, postural hypotension, excess sweating,
Metab.:
marked ↓ in REM sleep. Anticholinergic effects. Block antihypertensive
Excretion, t_:
effects of guanethidine. Enhance effects of some sympathomimetics. Can
be extremely toxic when combined w/MAO inhibs (but can also be done Toxicity/S.E.s: Headache, drowsiness, dry mouth, weight gain, postural
safely). Potentiates effects of alcohol and other CNS depressants. hypotension (central α2), sexual disturbances, liver damage,
Overdoses → coma, seizures, hypotension, depressed resp., arrhythmias. hyperpyrexia. Interactions w/TCAs, dextromethorphan,
Utility: Treat endogenous depression, enuresis, chronic pain, panic rxns, phobic meperidine, and tyramine can be fatal.
anxiety. Utility: Treat depression.
Special Features: TCAs preferred over MAOIs for initial treatment of endogenous Special Features: Usu. prescribed as alt. only when other drugs are ineffective.
depression. Severely depressed patients should never be
given more than a 1 week supply of a TCA (danger of
overdose).

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Name: Tranylcypromine (Parnate) Name: Fluoxetine (Prozac)
Class: Psychopharmacological Agents (Antidepressant) (MAOI) (Non-Hydrazine Class: Psychopharmacological Agents (Antidepressant) (SSRI)
Deriv.) Mech.: Blocks reuptake of serotonin.
Mech.: Inhib. of MAO → central build-up of NE, 5HT, DA. Absorption:
Absorption: Dist.:
Dist.: Metab.:
Metab.: Excretion, t_:
Excretion, t_: Toxicity/S.E.s: Anxiety, insomnia, restlessness, GI distress.
Toxicity/S.E.s: Headache, drowsiness, dry mouth, weight gain, postural Utility: Treat depression.
hypotension (central α2), sexual disturbances, liver damage, Special Features:
hyperpyrexia. Interactions w/TCAs, dextromethorphan, mepiridine,
and tyramine can be fatal.
Utility: Treat depression.
Special Features: Usu. prescribed as alt. only when other drugs are ineffective.

Name: Sertraline (Zoloft) Name: Lithium Carbonate


Class: Psychopharmacological Agents (Mood Stabilizer)
Class: Psychopharmacological Agents (Antidepressant) (SSRI) Mech.: Unknown, but may involve electrolyte/ion transport, enhanced reuptake of
Mech.: Blocks reuptake of serotonin. tryptophan → ↑ brain 5HT levels, inhib. of phosphatidyl inositol 2nd
Absorption: messenger system, ↓ DA & NE turnover, or ↑ synth. of ACh.
Dist.: Absorption:
Metab.: Dist.:
Metab.:
Excretion, t_:
Excretion, t_:
Toxicity/S.E.s: Anxiety, insomnia, restlessness, GI distress. Toxicity/S.E.s: Low TI (plasma levels must be monitored). Edema, sedation, fine
Utility: Treat depression. tremor (treat w/propranolol), polyuria, thirst, gastric upset, mild
Special Features: diarrhea. Serious = coarse tremor, vomiting, profuse diarrhea,
ataxia, cardiac arrhythmias, seizures, coma, death. ↓ thyroid fxn,
but usu. asympt. Diuretics → Na+ depletion → ↑ Li+ conc.
Utility: Prophylaxis for bipolar illness. Acute severe mania is more quickly
controlled w/neuroleptics. Combination therapy often required.
Special Features:

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Name: Scopolamine (Transderm-Scop) Name: Dimenhydrinate (Dramamine)
Class: Tertiary M2-Muscarinic Antagonist Class: Antiemetic (H1-Histamine Antagonist) (OTC)
Mech.: Bind to muscarinic receptors and competitively inhib. ACh interaction. Mech.: Competitive inhib. of histamine and histamine receptor interaction.
Absorption: Oral, transdermal, parenteral. Absorption: Oral, suppository.
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: Drowsiness, blurred vision, dry mouth, urinary retention, Toxicity/S.E.s: Drowsiness (marked in some patients). Mild anticholinergic
tachycardia, constipation, cycloplegia. Mostly avoided effects.
w/transdermal application. Utility: Prevent motion sickness. Can be used for morning sickness. Vertigo.
Utility: Prevent motion sickness (transdermal patch). Give parenterally in Special Features: Best if admin. prophylactically.
advance to counteract nasty anesthesia side effects (cardiac slowing,
salivation, bronchial secretions).
Features: In addition to atropine-like anti-musc properties, also produces central
depressant and anti-motion sickness effects. Best if admin.
prophylactically.

Name: Promethazine (Phenergan, Remsed) Name: Metoclopramide (Reglan)


Class: Antiemetic (H1-Histamine Antagonist) (OTC) Class: Antiemetic
Mech.: Competitive inhib. of histamine and histamine receptor interaction. Mech.: Cholinomimetic action → ↑ GI motility. Potent DA antagonism →
Absorption: Oral, suppository. blockade of DA receptors in CTZ and GI. Prob. also depresses vomiting
Dist.: center.
Metab.: Absorption: Oral
Excretion, t_: Dist.:
Toxicity/S.E.s: More drowsiness than other antihistamines. Mild anticholinergic Metab.:
effects. Excretion, t_:
Utility: Prevent motion sickness. Can be used for morning sickness. Vertigo. Toxicity/S.E.s: Somnolence, nervousness, dystonic rxns. Some Parkinsonism &
Special Features: May be effective in motion sickness when other antihistamines tardive dyskinesia. Some prolactin release.
are not. Best if admin. prophylactically. Utility: Antiemetic, esp. w/cancer chemotherapy, and emergency surgery/labor to
prevent aspiration of gastric contents.
Special Features: Best if admin. prophylactically.

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Name: Prochlorperazine (Compazine) Name: Ondansetron (Zofran)
Class: Antiemetic (Phenothiazine) Class: Antiemetic (5HT3 Antagonist)
Mech.: Blocks DA receptors in CTZ and GI tract. Probably also depresses Mech.:
vomiting center somewhat. Absorption: IV
Absorption: Oral, suppository. Dist.:
Dist.: Metab.:
Metab.: Excretion, t_:
Excretion, t_: Toxicity/S.E.s:
Toxicity/S.E.s: Drowsiness, hypotension. Hypersens—blood dyscrasias, Utility: Treat nausea/vomiting due to cancer chemotherapy.
jaundice, skin rashes. Dystonias, dyskinesias, Parkinsonism
(more often Special Features: Best if admin. prophylactically.
than w/chlorpromazine).
Utility: Antiemetic for drugs, radiation, uremia, pain, post-op, emotional, GI
irritation, cancer chemotherapy. Also very effective for intractable
hiccoughs.
Special Features: Best if admin. prophylactically.

Name: Dronabinol (Marinol, THC) Name: Ipecac


Class: Antiemetic (Cannabinoid)
Mech.: Class: Emetic
Absorption: Mech.:
Dist.: Absorption: Oral.
Metab.:
Dist.:
Excretion, t_:
Toxicity/S.E.s: High doses → impaired motor fxn. Mild tolerance, mild phys. Metab.:
dependence, psych. dependence. W/drawal → mild anorexia, insomnia, Excretion, t_:
irritability. Acute intoxication → hallucinations, delusions, paranoia, Toxicity/S.E.s:
anxiety. Utility: Induces vomiting.
Utility: Treat nausea & vomiting assoc. w/cancer chemotherapy. Best if admin. Special Features: Do not use to treat poisoning due to convulsants (e.g.,
prophylactically. Taken to produce relaxed euphoria, impaired attention, TCAs). Seizures may occur → ↑ risk of aspiration.
fantasy state, impaired depth perception.
Features: Hashish = Unadulterated resin from Cannabis plants. Smoked or
eaten. Far more potent than marijuana. Involved in the etymology of
“assassin” (An ancient Muslim sect regularly killed its enemies after
eating/smoking hashish → hashshashin).

22 www.brain101.info
Name: LSD Name: Phencyclidine (PCP)
Class: Hallucinogen Class: Hallucinogen
Mech.: Mech.:
Absorption: Absorption:
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: Mild tolerance, psychological dependence. No physical Toxicity/S.E.s: Impaired judgment, aggressive behavior, hostility. Mild tolerance,
dependence, no w/drawal syndrome. Acute intoxication → severe psychological dependence. No physical dependence, no w/drawal
sensory disturbances, panic, impaired org. of thinking, organic syndrome. Acute intoxication → muscle rigidity, convulsions,
brain syndrome, flashbacks. coma, psychosis, delirium, paranoia.
Utility: Euphoria w/more stimulation than relaxation. Utility:
Special Features: Special Features:

Name: Methamphetamine (Desoxyn, various street names)


Class: CNS-Active Sympathomimetic Agent (Indirect)
Mech.: Release of DA, NE, & 5HT from nerve terminals. Some blockade of
reuptake of DA, NE, & 5HT. Weak inhib. of MAO. Produces elev. of
mood, euphoria, ↑ alertness, ↓ sense of fatigue, ↓ food intake, periph.
sympathomimetic effects.
Absorption: Oral → good bioavail. “I want, once and for all, not to know many things.
Dist.: Crosses BBB.
Metab.: Wisdom sets limits to knowledge too”.
Excretion, t_:
Toxicity/S.E.s: Neurosis, paranoia, frank psychosis. Tolerance, but not as
strong as opiates. Acute toxicity → hypertension, stroke, seizures, cardiac
arrhythmias. Very strong psych. dependence. Mild physical dependence.
W/drawal → ↑ appetite, fatigue, depression. - Friedrich Nietzsche
Utility: Treat narcolepsy, ADHD. Off-label uses. Ice = smokable version.
Special Features: Not metab. by COMT. Decreased metab. by MAO. Higher
ratio of CNS/PNS actions than amphetamine.

23 www.brain101.info